ChEMBL ligand: CHEMBL592652 (GSK0660)
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869] There should be some charts here, you may need to enable JavaScript!
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181] Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396] There should be some charts here, you may need to enable JavaScript!
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
ChEMBL	Displacement of [3H]GW2433 from human PPARalpha receptor by ligand displacement assay	B	5	pIC50	>10000	nM	IC50	J Med Chem (2010) 53: 1857-1861 [PMID:20128594]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
ChEMBL	Binding affinity to PPARdelta (unknown origin) assessed as inhibition constant by TR-FRET based LanthaScreen competitive binding assay	B	8.28	pKi	5.2	nM	Ki	J Med Chem (2023) 66: 4961-4978 [PMID:36967575]
ChEMBL	Binding affinity to PPAR-delta (unknown origin) by TR-FRET assay	B	8.33	pKi	4.65	nM	Ki	J Med Chem (2020) 63: 16012-16027 [PMID:33325691]
ChEMBL	Antagonist activity at human PPARdelta ligand binding domain-mediated transcriptional activity in CV1 cells by Gal4 chimera reporter assay	B	6.5	pIC50	316.23	nM	IC50	J Med Chem (2010) 53: 1857-1861 [PMID:20128594]
GtoPdb	-	-	6.5	pIC50	300	nM	IC50	Mol Endocrinol (2008) 22: 523-9 [PMID:17975020]
ChEMBL	Inhibition of human PPARdelta receptor by ligand displacement assay	B	6.8	pIC50	158.49	nM	IC50	J Med Chem (2010) 53: 1857-1861 [PMID:20128594]
ChEMBL	Binding affinity to N-terminal hexa-histidine tagged and fluorescein-labeled human PPAR-beta/delta (164 to 441 residues) expressed in Escherichia coli BL21-DE3 incubated for 1 hr by fluorescence anisotropy	B	6.81	pIC50	155	nM	IC50	Eur J Med Chem (2015) 94: 229-236 [PMID:25768705]
ChEMBL	Antagonist activity at PPARdelta LBD (unknown origin) assessed as increase in recruitment of SMRT ID2 corepressor peptide by TR-FRET assay	B	5.27	pEC50	5400	nM	EC50	Bioorg Med Chem (2020) 28: 115226-115226 [PMID:31806266]
ChEMBL	Antagonist activity at PPARdelta LBD (unknown origin) assessed as increase in recruitment of SMRT ID2 corepressor peptide by TR-FRET assay	B	5.36	pEC50	4340	nM	EC50	J Med Chem (2020) 63: 16012-16027 [PMID:33325691]
ChEMBL	Antagonist at PPARdelta LBD (unknown origin) assessed as increase in recruitment of coactivator peptide C33 cotreated with PPARdelta agonist GW501516 by TR-FRET assay	B	5.4	pEC50	4000	nM	EC50	Bioorg Med Chem (2020) 28: 115226-115226 [PMID:31806266]
ChEMBL	Antagonist activity at PPARdelta LBD (unknown origin) assessed as increase in fluorescein labeled SMRT-ID2 corepressor peptide requirement by TR-FRET assay	B	5.44	pEC50	3620	nM	EC50	J Med Chem (2023) 66: 4961-4978 [PMID:36967575]
ChEMBL	Antagonist activity at PPARdelta (unknown origin) by TR-FRET assay	B	5.47	pEC50	3400	nM	EC50	ACS Med Chem Lett (2022) 13: 1131-1136 [PMID:35859875]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396]
ChEMBL	Displacement of fluormone Pan-PPAR Green from mouse recombinant GST-tagged PPARbeta/delta LBD after 60 mins by TR-FRET assay	B	6.52	pIC50	>=300	nM	IC50	J Med Chem (2012) 55: 2858-2868 [PMID:22369181]
ChEMBL	Inverse agonist activity at PPARbeta/delta in mouse C2C12 cells assessed as inhibition of Angptl4 expression after 24 hrs by RT-qPCR analysis	F	7.32	pIC50	48	nM	IC50	J Med Chem (2012) 55: 2858-2868 [PMID:22369181]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL	Inhibition of human PPARgamma receptor by ligand displacement assay	B	5	pIC50	>10000	nM	IC50	J Med Chem (2010) 53: 1857-1861 [PMID:20128594]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]